51085-95-1Relevant academic research and scientific papers
PROTEIN KINASE D INHIBITORS
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Page/Page column 62; 73, (2012/06/30)
Compounds according to Formula (I), are potent inhibitors of protein kinase D (pan-PKD) activity. PKD controls key signaling cascades in cells, affecting cell proliferation, gene transcription, and protein trafficking. Accordingly, pharmaceutically acceptable compositions of the inventive compounds are candidate therapeutics for pathological conditions conditioned by changes in PKD activity.
From pyrroles to 1-oxo-2,3,4,9-tetrahydro-1H-β-carbolines: A new class of orally bioavailable mGluR1 antagonists
Fabio, Romano Di,Micheli, Fabrizio,Alvaro, Giuseppe,Cavanni, Paolo,Donati, Daniele,Gagliardi, Tatiana,Fontana, Gabriele,Giovannini, Riccardo,Maffeis, Micaela,Mingardi, Anna,Tranquillini, Maria Elvira,Vitulli, Giovanni
, p. 2254 - 2259 (2008/02/03)
Exploiting the SAR of the known pyrrole derivatives, a new class of mGluR1 antagonists was designed by replacement of the pyrrole core with an indole scaffold and consequent cyclization of the C-2 position into a tricyclic β-carboline template. The appropriate exploration of the position C-6 with a combination of H-bond acceptor groups coupled with bulky/lipophilic moieties led to the discovery of a new series of mGluR1 antagonists. These compounds exhibited a non-competitive behavior, excellent pharmacokinetic properties, and good in vivo activity in animal models of acute and chronic pain, after oral administration.
